反应条件
1: 43 percent / H2SO4 / 2 h / Heating 2: 99 percent / LiBH4 / tetrahydrofuran / 2.5 h / 0 - 20 °C 3: 52 percent / Et3N; DBU / CH2Cl2 / 16 h / 20 °C 4: 95 percent / oxalyl chloride; DMSO; Et3N / CH2Cl2 / 1.5 h / -70 °C 5: 87 percent / tetrahydrofuran / 2 h / 0 °C 6: 77 percent / PdCl2(PPh3)2; Bu3SnH / H2O; CH2Cl2 / 16 h / 20 °C 7: Et3N / tetrahydrofuran; H2O / 2 h / 20 °C 8: 94 percent / TBAF / tetrahydrofuran / 0.5 h / 0 - 20 °C 9: 61 percent / SnCl2*2H2O / methanol / 0.75 h / Heating 10: 50 percent / pyridine / CH2Cl2 / 2.5 h / 20 °C 11: 32 percent / NMO; 4 Angstroem molecular sieves; TPAP / CH2Cl2; acetonitrile / 2.5 h / 20 °C 12: 77 percent / PPh3; pyrrolidine; Pd(PPh3)4 / CH2Cl2; acetonitrile / 2.25 h / 20 °C View Scheme
参考文献
Gregson; Howard; Hartley; Brooks; Adams; Jenkins; Kelland; Thurston
Journal of Medicinal Chemistry, 2001 , vol. 44, # 5 p. 737 - 748